PE20020258A1 - DERIVATIVES OF 4-PHENYL-PYRIDINE AS ANTAGONISTS OF THE NEUROQUININ 1 (NK-1) RECEPTOR - Google Patents

DERIVATIVES OF 4-PHENYL-PYRIDINE AS ANTAGONISTS OF THE NEUROQUININ 1 (NK-1) RECEPTOR

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Publication number
PE20020258A1
PE20020258A1 PE2001000730A PE2001000730A PE20020258A1 PE 20020258 A1 PE20020258 A1 PE 20020258A1 PE 2001000730 A PE2001000730 A PE 2001000730A PE 2001000730 A PE2001000730 A PE 2001000730A PE 20020258 A1 PE20020258 A1 PE 20020258A1
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Peru
Prior art keywords
phenyl
pyridine
methyl
neuroquinin
antagonists
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Application number
PE2001000730A
Other languages
Spanish (es)
Inventor
Torsten Hoffmann
Patrick Schnider
Heinz Stadler
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Hoffmann La Roche
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Publication of PE20020258A1 publication Critical patent/PE20020258A1/en

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 4-FENIL-PIRIDINA DE FORMULA IA, IB DONDE R1 ES EL GRUPO a, b, ENTRE OTROS; o ES -NH(CH2)2OH, -NR3C(O)CH3, NR3-C(O)-CICLOPROPILO; R2 ES METILO, Cl; R3 ES H, METILO; R ES H, -(CH2)2OH; n ES 1-2. SON COMPUESTOS PREFERIDOS N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-N-METIL-4-o-TOLIL-6-[1,2,4]TRIAZOL-1-IL-NICOTINAMIDA, N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-6-(2-HIDROXI-ETILAMINO)-N-METIL-o-TOLIL-NICOTINAMIDA, 2-(3,5-BIS-TRIFLUOROMETIL-FENIL)-N-[4-(2-CLORO-FENIL)-6-(2-HIDROXI-ETILAMINO)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA LA PREPARACION Y COMPUESTOS INTERMEDIOS. LOS DERIVADOS DE 4-FENIL-PIRIDINA SON ANTAGONISTAS DEL RECEPTOR DE NEUROQUININA 1 (NK-1) Y SON UTILES PARA EL TRATAMIENTO DE TRASTORNOS DEL SISTEMA NERVIOSO CENTRALREFERS TO COMPOUNDS DERIVED FROM 4-PHENYL-PYRIDINE FROM FORMULA IA, IB WHERE R1 IS GROUP a, b, AMONG OTHERS; or ES -NH (CH2) 2OH, -NR3C (O) CH3, NR3-C (O) -CYCLOPROPYL; R2 IS METHYL, Cl; R3 IS H, METHYL; R IS H, - (CH2) 2OH; n IS 1-2. PREFERRED COMPOUNDS ARE N- (3,5-BIS-TRIFLUOROMETHYL-BENZYL) -N-METHYL-4-o-TOLIL-6- [1,2,4] TRIAZOL-1-IL-NICOTINAMIDE, N- (3,5 -BIS-TRIFLUOROMETHYL-BENZYL) -6- (2-HYDROXY-ETHYLAMINE) -N-METHYL-o-TOLYL-NICOTINAMIDE, 2- (3,5-BIS-TRIFLUOROMETHYL-PHENYL) -N- [4- (2- CHLORO-PHENYL) -6- (2-HYDROXY-ETHYLAMINE) -PYRIDINE-3-IL] -N-METHYL-ISOBUTYRAMIDE, AMONG OTHERS. IT ALSO REFERS TO A PROCEDURE FOR THE PREPARATION AND INTERMEDIATE COMPOUNDS. 4-PHENYL-PYRIDINE DERIVATIVES ARE ANTAGONISTS OF THE NEUROQUININ 1 RECEPTOR (NK-1) AND ARE USEFUL FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS

PE2001000730A 2000-07-24 2001-07-18 DERIVATIVES OF 4-PHENYL-PYRIDINE AS ANTAGONISTS OF THE NEUROQUININ 1 (NK-1) RECEPTOR PE20020258A1 (en)

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EP00115846 2000-07-24

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US (2) US6576762B2 (en)
EP (1) EP1305319B1 (en)
JP (1) JP4118673B2 (en)
KR (1) KR100527214B1 (en)
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YU2803A (en) 2006-01-16
CY1106113T1 (en) 2011-06-08
ZA200300219B (en) 2004-04-08
NO20030353D0 (en) 2003-01-23
ECSP034446A (en) 2003-03-10
US20020038030A1 (en) 2002-03-28
GT200100148A (en) 2002-05-16
DE60118569D1 (en) 2006-05-18
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US6576762B2 (en) 2003-06-10
HK1058360A1 (en) 2004-05-14
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HU229231B1 (en) 2013-09-30
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MXPA03000367A (en) 2003-05-27
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CN1192032C (en) 2005-03-09
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